Development of Novel Indolyl-derived Biologically Active Compounds. Synthesis, Characterization and Applications as (Anti-MRSA, Anticancer)

      Аннотация: MRSA is a methicillin-resistance Staphylococcus aureus and a strain of Staphylococcus aureus that developed resistance to the killing effect of the ?-lactam antibiotics, which include the penicillins (methicillin, dicloxacillin, oxacillin, etc.), MRSA is sometimes called a “superbug” because it is very difficult to treat and it causes a huge number of infections every year in hospitals all over the world. The novel synthesized indoles will add a valuable new addition to the antibacterial arsenal for MRSA infections, it would be new bactericidal agents effective against resistant isolates or standard. We have shown for the first time that the cycloalkanoindoles,bis-indolobenzocarbazoles and the oxidized bis-indolylmethenes inhibited growth of drug resistant MRSA either standard or isolate and other Gram-positive bacteria at low concentrations. Some of these novel bis- and tris-indolyl compounds described in this work have been screened in the national cancer institute (NCI) in USA for one and five dose that showed the highest antipoliferative activity in a nanomolar scale towards the selected cancers cell lines (Non small lung: NCIeH460, Ovarian: OVCAR-4 and Breast: MCF).

Ключевые слова: Cycloalkanoindoles, bis-indolobenzocarbazoles, oxidized bis-indolylmethenes, bactericidal agents, gram-positive pathogens, MRSA, Superbug, antibiotics resistance, Anticancer agents, nanomolar active